Abstract：
:To assess the importance of the cysteine residues Cys347 and Cys351 in the carboxylic tail in the human D1 dopamine receptor, seven mutant receptors were constructed by PCR. The pharmacological and functional properties of the wild-type and mutant receptors were assessed following transient expression in COS-7 cells. Affinities for [3H]SCH 23390 of mutant S347 (Cys347-->Gly), T348 (Tyr348-->stop), S351 (Cys351-->Gly), T351 (Cys351-->stop), T352 (Pro352-->stop), and S347/S351 (Cys347-->Gly and Cys351-->Gly) were similar to that of wild-type receptor, whereas the expression levels were reduced up to 80%. The potency of dopaminergic antagonists for these mutant receptors was very similar to that of the wild-type receptor. However, mutant T347 (Cys347-->stop) showed a 15-25-fold reduced affinity for the antagonists SCH 23390, (+)-butaclamol, and cis-flupentixol, thus not allowing radioligand analysis. Wild-type and mutant receptors responded dose-dependently with similar potency to dopamine and SKF 38393 with an increased adenylyl cyclase activity. However, mutant receptors with the Cys347 residue changed or removed displayed a diminished ability to activate adenylyl cyclase. Dopamine preexposure desensitized wild-type and mutant S351 receptors. However, mutant receptors with Cys347 replaced or the distal part of the carboxyl tail removed were unable to desensitize. Thus, Cys347 in the cytoplasmic tail of the human D1 dopamine receptor is important for the receptor in maintaining the conformation for antagonist binding, to play a crucial role in activation of adenylyl cyclase, and to be essential for agonist-induced desensitization.
journal_name
J Neurochemjournal_title
Journal of neurochemistryauthors
Jensen AA,Pedersen UB,Kiemer A,Din N,Andersen PHdoi
10.1046/j.1471-4159.1995.65031325.xsubject
Has Abstractpub_date
1995-09-01 00:00:00pages
1325-31issue
3eissn
0022-3042issn
1471-4159journal_volume
65pub_type
杂志文章abstract：:In Guadeloupe, epidemiological data have linked atypical parkinsonism with fruit and herbal teas from plants of the Annonaceae family, particularly Annona muricata. These plants contain a class of powerful, lipophilic complex I inhibitors, the annonaceous acetogenins. To determine the neurotoxic potential of these sub...
journal_title：Journal of neurochemistry
pub_type： 杂志文章
doi：10.1046/j.1471-4159.2003.02138.x
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journal_title：Journal of neurochemistry
pub_type： 杂志文章
doi：10.1046/j.1471-4159.1998.71062322.x
更新日期：1998-12-01 00:00:00
abstract：:We have shown that following heat shock (42.5 degree C for 30 min), mouse-derived C1300 N2A neuroblastoma cells contain increased levels of mRNA coding for the inducible form of heat shock protein 70 and for ubiquitin. Incubation of C1300 cells with iron also induces an elevation in content of mRNAs coding for the sam...
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pub_type： 杂志文章
doi：10.1111/j.1471-4159.1993.tb03198.x
更新日期：1993-02-01 00:00:00
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pub_type： 杂志文章
doi：10.1046/j.1471-4159.1999.0721843.x
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journal_title：Journal of neurochemistry
pub_type： 杂志文章
doi：10.1046/j.1471-4159.1994.62062106.x
更新日期：1994-06-01 00:00:00
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journal_title：Journal of neurochemistry
pub_type： 杂志文章
doi：10.1111/j.1471-4159.1990.tb13286.x
更新日期：1990-01-01 00:00:00
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journal_title：Journal of neurochemistry
pub_type： 杂志文章
doi：10.1046/j.1471-4159.1998.70041532.x
更新日期：1998-04-01 00:00:00
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pub_type： 杂志文章
doi：10.1111/j.1471-4159.1990.tb04557.x
更新日期：1990-09-01 00:00:00
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pub_type： 杂志文章
doi：10.1111/j.1471-4159.1986.tb02828.x
更新日期：1986-07-01 00:00:00
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journal_title：Journal of neurochemistry
pub_type： 杂志文章
doi：10.1111/j.1471-4159.1984.tb06703.x
更新日期：1984-07-01 00:00:00
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journal_title：Journal of neurochemistry
pub_type： 杂志文章
doi：10.1111/j.1471-4159.1984.tb12832.x
更新日期：1984-10-01 00:00:00
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journal_title：Journal of neurochemistry
pub_type： 杂志文章
doi：10.1046/j.1471-4159.1996.66020685.x
更新日期：1996-02-01 00:00:00
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pub_type： 杂志文章,评审
doi：10.1111/jnc.14308
更新日期：2018-03-01 00:00:00
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journal_title：Journal of neurochemistry
pub_type： 杂志文章
doi：10.1111/jnc.12032
更新日期：2012-12-01 00:00:00
abstract：:The kinetics of the reactions of nine opioid peptides with the neutral endopeptidase ("enkephalinase") activities of human kidney, rat kidney, and rat brain have been determined. These opioid peptides can be divided into two classes, those that are good inhibitors of Leu5-enkephalin hydrolysis (Ki less than 75 microM)...
journal_title：Journal of neurochemistry
pub_type： 杂志文章
doi：10.1111/j.1471-4159.1984.tb00925.x
更新日期：1984-08-01 00:00:00
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journal_title：Journal of neurochemistry
pub_type： 杂志文章
doi：10.1046/j.1471-4159.1995.65020818.x
更新日期：1995-08-01 00:00:00
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pub_type： 杂志文章,评审
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更新日期：2013-05-01 00:00:00
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journal_title：Journal of neurochemistry
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journal_title：Journal of neurochemistry
pub_type： 杂志文章
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更新日期：2000-10-01 00:00:00
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pub_type： 杂志文章
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更新日期：2005-07-01 00:00:00
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pub_type： 杂志文章
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更新日期：2010-08-01 00:00:00
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journal_title：Journal of neurochemistry
pub_type： 杂志文章
doi：10.1046/j.1471-4159.1994.63031003.x
更新日期：1994-09-01 00:00:00
abstract：:Rats with unilateral lesions of the locus coeruleus were used to study the role of norepinephrine (NE) signal input in the down-regulation by antidepressants of the noradrenergic cyclic AMP-generating system in the cortex. Chronic administration of both desipramine (blockade of NE reuptake) and iprindole (no blockade ...
journal_title：Journal of neurochemistry
pub_type： 杂志文章
doi：10.1111/j.1471-4159.1982.tb04739.x
更新日期：1982-07-01 00:00:00
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journal_title：Journal of neurochemistry
pub_type： 杂志文章
doi：10.1111/j.1471-4159.1985.tb10526.x
更新日期：1985-12-01 00:00:00
abstract：:The turnover rate of gamma-aminobutyric acid (GABA) in the rat striatum was estimated by measuring its accumulation after inhibition of GABA-transaminase (GABA-T) with gabaculine. Intrastriatal injections of 100 micrograms gabaculine induced a rapid and complete inhibition of GABA-T. GABA accumulation was linear with ...
journal_title：Journal of neurochemistry
pub_type： 杂志文章
doi：10.1111/j.1471-4159.1984.tb09720.x
更新日期：1984-01-01 00:00:00
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journal_title：Journal of neurochemistry
pub_type： 杂志文章
doi：10.1111/j.1471-4159.1985.tb05447.x
更新日期：1985-02-01 00:00:00
abstract：:Null mutations in progranulin (GRN) are associated with frontotemporal lobar degeneration characterized by intraneuronal accumulation of TAR DNA-binding protein-43 (TDP-43). However, the mechanism by which GRN deficiency leads to neurodegeneration remains largely unknown. In primary cortical neurons derived from Grn k...
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pub_type： 杂志文章
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更新日期：2010-11-01 00:00:00
